Chemistry:GYKI 52895

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Short description: Chemical compound
GYKI 52895
GYKI 52895.svg
GYKI-52895-3d.png
Clinical data
Other names4-(8,9-Dihydro-8-methyl-7H-1,3-dioxolo[4,5-h][2,3]benzodiazepin-5-yl)benzenamine
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
FormulaC17H17N3O2
Molar mass295.342 g·mol−1
3D model (JSmol)
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GYKI 52895 is a drug which is a 2,3-benzodiazepine derivative that also shares the 3,4-methylenedioxyamphetamine pharmacophore. Unlike other similar drugs, GYKI 52895 is a selective dopamine reuptake inhibitor (DARI),[1][2] which appears to have an atypical mode of action compared to other DARIs.[3] Its DRI activity is shared by numerous addictive drugs including amphetamine and its derivatives (e.g. dextromethamphetamine), cocaine, and methylphenidate and its derivatives (e.g. ethylphenidate). However, dopaminergic drugs are also prone to producing emetic effects such as in the case of apomorphine.

Egis Pharmaceuticals began clinical development of the drug in 1997 for major depressive disorder and Parkinson's disease, but it was discontinued in 2001.[4]

See also

References

  1. "Pharmacological Effects of GYKI 52895, a New Selective Dopamine Uptake Inhibitor.". European Journal of Pharmacology 183 (4): 1416–1417. 1990. doi:10.1016/0014-2999(90)94548-C. 
  2. "Modulation of dopamine transporter activity by nicotinic acetylcholine receptors and membrane depolarization in rat pheochromocytoma PC12 cells". Journal of Neurochemistry 72 (6): 2437–44. June 1999. doi:10.1046/j.1471-4159.1999.0722437.x. PMID 10349853. 
  3. "Novel pathway for an old neurotransmitter: dopamine-induced neuronal calcium signalling via receptor-independent mechanisms". Cell Calcium 48 (2–3): 176–82. 2010. doi:10.1016/j.ceca.2010.08.008. PMID 20846720. 
  4. "GYKI 52895". Adis Insight. https://adisinsight.springer.com/drugs/800001417.